title: Synergistic encapsulation of the anti-HIV agent efavirenz within mixed poloxamine/poloxamer polymeric micelles.
abstract: This study investigated the synergistic performance of mixed polymeric micelles made of linear and branched poly(ethylene oxide)-poly(propylene oxide) for the more effective encapsulation of the anti-HIV drug efavirenz. The co-micellization process of 10% binary systems combining different weight ratios of a highly hydrophilic poloxamer (Pluronic F127) and a more hydrophobic poloxamine counterpart (Tetronic T304 and T904) was investigated by means of dynamic light scattering, cloud point and electronic spin resonance experiments. Then, the synergistic solubilization capacity of the micelles was shown. Findings revealed a sharp solubility increase from 4 μg/ml up to more than 33 mg/ml, representing a 8430-fold increase. Moreover, the drug-loaded mixed micelles displayed increased physical stability over time in comparison with pure poloxamine ones. Overall findings confirmed the enormous versatility of the poloxamer/poloxamine systems as Trojan nanocarriers for drug encapsulation and release by the oral route and they entail a relevant enhancement of the previous art towards a more compliant pediatric HIV pharmacotherapy.
authors.affiliation: The Group of Biomaterials and Nanotechnology for Improved Medicines (BIONIMED), Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Argentina.
authors.forename: Diego A
authors.initials: DA
authors.lastname: Chiappetta
authors.forename: Graciela
authors.initials: G
authors.lastname: Facorro
authors.forename: Emilio Rubin
authors.initials: ER
authors.lastname: de Celis
authors.forename: Alejandro
authors.initials: A
authors.lastname: Sosnik
mesh_terms: D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy; D000480:Alkynes; D019380:Anti-HIV Agents / Q000008:administration & dosage* / Q000737:chemistry; D048588:Benzoxazines / Q000008:administration & dosage* / Q000737:chemistry; D003521:Cyclopropanes; D016503:Drug Delivery Systems; D004357:Drug Synergism; D005029:Ethylenediamines / Q000737:chemistry*; D006678:HIV / Q000187:drug effects*; D006801:Humans; D008823:Micelles; D053769:Nanocapsules / Q000737:chemistry*; D020442:Poloxamer / Q000737:chemistry*; D012995:Solubility / Q000187:drug effects
chemical_list: D000480:Alkynes; D019380:Anti-HIV Agents; D048588:Benzoxazines; D003521:Cyclopropanes; D005029:Ethylenediamines; D008823:Micelles; D053769:Nanocapsules; C525597:Tetronic 904; D020442:Poloxamer; C098320:efavirenz